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Role Assessment of Water-Soluble Pharmaceutical Form of Phosphatidylcholine on the Catalytic Activity of Cytochrome P450 2C9 and 2D6.
Int J Mol Sci
December 2024
Institute of Biomedical Chemistry, Pogodinskaya Street, 10, Build 8, 119121 Moscow, Russia.
This study aimed to investigate whether the water-soluble pharmaceutical form of phosphatidylcholine nanoparticles (wPC) stimulated the catalytic activity of CYP enzymes 2C9 and 2D6. We have shown that electroenzymatic CYP2C9 catalysis to nonsteroidal anti-inflammatory drug naproxen as a substrate was enhanced from 100% to 155% in the presence of wPC in media. Electroenzymatic CYP2D6 activity in the presence of the adrenoceptor-blocking agent bisoprolol as a substrate was elevated significantly from 100% to 144% when wPC was added to potassium phosphate buffer solution.
View Article and Find Full Text PDFNyctohemeral effects of topical beta-adrenoceptor blocking agents measured with an intraocular telemetry sensor.
Br J Ophthalmol
November 2024
Hamilton Glaucoma Center, Shiley Eye Institute and Department of Ophthalmology, University of California, La Jolla, California, USA.
Objective: To evaluate nyctohemeral effects of topical beta-adrenoceptor blocking agents and their fixed combinations on intraocular pressure (IOP) in patients with primary open-angle glaucoma implanted with an ocular telemetry sensor.
Methods: 22 patients who had previously been implanted with a sulcus-based IOP sensor (eyemate) were included in this prospective clinical trial. Three classes of medications were analysed: beta-blockers (BB), fixed combination of BB and carbonic anhydrase inhibitors (BB-CAI), and combinations of BB and prostaglandin analogues (BB-PGAs).
Genetic Insights Into Perinatal Outcomes of Maternal Antihypertensive Therapy During Pregnancy.
JAMA Netw Open
August 2024
Medical Research Council Integrative Epidemiology Unit, University of Bristol, Bristol, United Kingdom.
Importance: Limited information exists regarding the impact of pharmacotherapy in pregnancy due to ethical concerns of unintended fetal harm. Yet, maternal prescriptive drug use for chronic conditions such as hypertension is common.
Objective: To investigate potential causal relationships between perturbing maternal genetic variants influencing antihypertensive drug targets and perinatal outcomes among offspring using mendelian randomization (MR).
Han Chinese specific cytochrome P450 polymorphisms and their impact on the metabolism of anti-hypertensive drugs with adrenoreceptor blocking properties.
Expert Opin Drug Metab Toxicol
June 2021
School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou Zhejiang, P.R. China.
: Cytochrome P450 (CYP) is a monooxygenase superfamily mediating the elimination of anti-hypertensive drugs. Polymorphisms of CYP would lead to differential drug efficacy. Building relationships between genotype and phenotype will benefit individual medical treatment of hypertension.
View Article and Find Full Text PDFBetaxolol: A comprehensive profile.
Profiles Drug Subst Excip Relat Methodol
February 2021
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Kingdom of Saudi Arabia. Electronic address:
Betaxolol is a relatively cardioselective β-adrenoceptor blocking drug, with no partial agonist (intrinsic sympathomimetic) activity and weak membrane-stabilizing (local anesthetic) activity. Betaxolol selectively and competitively binds to and blocks beta-1 (β1) adrenergic receptors in the heart, thereby decreasing cardiac contractility and rate. This leads to a reduction in cardiac output and lowers blood pressure.
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